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68 Cards in this Set

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diuretics
thiazides (hydrochlorothiazide)

loop diuretics (furosemide)

k sparing diuretics (spironolactone)
Inhibitors of the RAA system
ACE inhibitors (lisinopril)

angiotensin receptor blockers (losartan)
Vasodilators
direct acting (nitroprusside and hydralazine)

calcium entry blockers (verapamil, nifedipine)
Sympatholytic agents
act within CNS (clonidine)

act on autonomic ganglia (trimethaphan)

act on post-ganglionic neurons (reserpine)

block peripheral adrenergic receptors (atenolol, prazosin, labetolol)
Drug class of hydrocholorothiazide
(HydroDiuril)
pharmacologic class - thiazide diuretic

therapeutic class - diuretic, antihypertensive
Pharmacodynamics of hydrochlorothiazide
blocks the reuptake of Cl and Na from tubular fluid after glomerular filtration; also appears to cause decrease in SVR, unclear mechanism; will lower BP by up to 10-15mm in may patients; is useful as a monotherapy or in combinations
Pharmacokinetics of hydrochlorothiazide
F - 70%, excreted unchanged in urine; short half-life (hours); HCTZ not available in IV formulation; onset 2 hours, peak 5 hours, duration 10 hours
Toxicity of hydrochlorothiazide
allergy to sulfa antibiotics; cause K and Mg depletion; cause Na and Cl depletion, metabolic alkalosis; volume depletion; worsen hyperuricemia
Interactions of hydrochlorothiazide
additive effects with most other antihypertensives
Special considerations for hydrochlorothiazide
more side effects in geriatric patients; pregnancy class D; ineffective in patients with significant renal disease
Indications and dose/route with hydrochlorothiazide
12.5 mg or 25 mg po every morning; little benefit (more toxicity) when given in higher doses
Monitoring of hydrochlorothiazide
BP, weight, edema, K, Mg, BUN, creatinine
Lisinopril
(Prinivil; also captopril, enalapril, ramipril)
Drug class of lisinopril
pharmacologic class - ACE inhibitor; therapeutic antihypertensive, treatment of CHF, preserving renal function, preserving LV function after MI, acute management of MI
Pharmacodynamics of Lisinopril
inhibits the conversion of AT I to AT II by ACE; diminishes both vasocontriction and stimulation of aldosterone secretion by AT II
Pharmacokinetics of Lisinopril
well absorbed; onset 1 hour, peak 6 hours, duration 24 hours; once a day is fine; excreted primarily in urine as unchanged drug
Toxicity of lisinopril
orthostatic hypotension; use with caution in patients with impaired renal function, or renal artery stenosis; be careful in patients on diuretics, or those with aortic stenosis; angioedema; acute renal failure
Interactions of lisinopril
additive effects with most other antihypertensives; NSAIDS may reduce ability to lower BP; hyperkalemia with KCL, others;
Special considerations of lisinopril
often discontinue diuretics prior to beginning use to reduce hypotension; category C/D in pregnancy, abnormal cartilage development
Indications and dose/route of lisinopril
begin 10mg per day, titrate slowly upward to 40 mg per day max
Monitoring of lisinopril
BP, weight, edema, K, BUN, creatinine, cough
Losartan
(CoZaar, also irbesartan, etc)
Drug Class of Losartan
pharmacologic class: angiotensin I receptor blocker (ARB)

therapeutic class: diuretic, antihypertensive, preserve renal function, treatment of CHF
Pharmacodynamics of Losartan
block stimulation of AT I receptor by angiotensin II, thereby reducing vasoconstriction and productiong of aldosterone
Pharmacokinetics of Losartan
F ~ 30%; onset 6 hours; extensive first pass effect; active metabolite is 40x more potent, much longer half-life
Toxicity of Losartan
dizziness; orthostatic hypotension; worsening of renal failure
Interactions of Losartan
additive effects with most other antihypertensives
Special considerations of Losartan
pregnancy class C/D; use care in patients on diuretics, those with renal artery stenosis, those with mitral or aortic stenosis
Indications and dose/route
1 for hypertension, daily doses 25-100mg every day
Special considerations for hydrochlorothiazide
more side effects in geriatric patients; pregnancy class D; ineffective in patients with significant renal disease
Indications and dose/route with hydrochlorothiazide
12.5 mg or 25 mg po every morning; little benefit (more toxicity) when given in higher doses
Monitoring of hydrochlorothiazide
BP, weight, edema, K, Mg, BUN, creatinine
Lisinopril
(Prinivil; also captopril, enalapril, ramipril)
Drug class of lisinopril
pharmacologic class - ACE inhibitor; therapeutic antihypertensive, treatment of CHF, preserving renal function, preserving LV function after MI, acute management of MI
Pharmacodynamics of Losartan
block stimulation of AT I receptor by angiotensin II, thereby reducing vasoconstriction and production of aldosterone
Pharmacokinetics of Losartan
F ~ 30%; onset 6 hours; extensive first pass effect; active metabolite in 40x more potent, much longer half-life
Toxicity of Losartan
dizziness, orthostatic hypotension; worsening of renal failure
Interactions of Losartan
additive effects with most other antihypertensives
Special considerations of Losartan
pregnancy class C/D; use care in patients on diuretics, those with renal artery stenosis; those with mitral or aortic stenosis
Indications and dose/route of Losartan
1 for HTN, daily doses 25-100mg every day
Monitoring of Losartan
BP, weight, edema, electrolytes, BUN, and creatinine
Nitroprusside
Nipride, Nitropress
Drug class of nitroprusside
pharmacologic vasodilator

therapeutic class: antihypertensive, management of CHF, management of pulmonary hypertension, produce controlled hypotension to reduce bleeding during surgery
Pharmacodynamics of nitroprusside
acts "directly" on vascular smooth muscle to cause dilatation of both veins and arterioles; metabolized to release CN- and NO, which activates guanylate cyclase, leads to production of cGMP from GTP, which then leads to vasodilation; cGMP then hydrolzed to GMP by PDE
Pharmacokinetics of nitroprusside
only route is via iv; rapid onset (minutes) and cessation (minutes), thereby allowing minute-by-minute titration; CN- metabolite is converted to SCN in the liver, then excreted in the urine; must be given by continuous infusion
Toxicity of nitroprusside
excessive hypotension; accumulation of CN and thiocyanate; headache; decreased blood flow to brain
Interactions of nitroprusside
additive effects with most other antihypertensives
Special considerations of nitroprusside
monitor very closely; avoid high infusion rates or prolonged infusions, to prevent accumulation of CN-; use with caution in patients with increase intracranial pressure
Indications and dose/route of nitroprusside
for treatment of hypertensive crisis, given as IV infusion at 0.3-10 mcg/kg per minute; do not exceed 24 hours of infusion
Monitoring of nitroprusside
BP, HR, metabolic acidosis; most often requires an arterial line
Hydralazine
apresoline
Drug class of hydralazine
pharmacologic class: peripheral vasodilator

therapeutic class: antihypertensive, treatment of CHF, vasodilator
Pharmacodynamics of hydralazine
"direct" acting vasodilator; may act by inducing endothelium to produce NO, which then passes to SM cells and induces production of cGMP, minimal venodilating effect
Pharmacokinetics of hydralazine
given po, im, iv; metabolized extensively in GI mucosa and in the liver; eventually excreted as metabolites in urine; F ~ 40%; onset 30 after po dose, 10 minutes after iv dose; persist for 2-6 hours
Toxicity of hydralazine
more dangerous in patients with renal disease, prior to stroke, angina; watch for hypotension, edema, occasionally drug induced lupus
Interactions of hydralazine
additive effects with most other antihypertensives
Special considerations of hydralazine
never use as a monotherapy for treatment of hypertension, since edema and reflex tachcardia will result, concert giving to patients with CAD
Indications and dose/route of hydralazine
dose 10-50mg po four times daily
Monitoring hydralazine
BP, weight, edema, BUN, creatinine, symptoms of lupus or angina
Verapamil
Isoptin, Calan, similar to nifedipine, amlodipine, diltiazem, etc
Drug class of verapamil
pharmacologic class: calcium entry blocker

therapeutic class: antihypertensive, antianginal, and antiarrhythmic
Pharmacodynamics of verapamil
reduces BP by inhibiting influx of calcium through "slow channels", thereby dilating peripheral arterioles; produces negative inotropic effect as well; for angina, reduces afterload, thus decreasing oxygen consumption; also, inhibits spasm of coronary arteries in vasospastic angina; blocks re-entry paths through AV node in paroxysmal SVT
Pharmacokinetics of verapamil
absorbed rapidly, but F ~ 30%
also available in SR tablets; cleared by kidney and liver (produces active metabolites); onset 2 hours po, 1-5 min iv; half-life 6-12 hours; may be given po or iv
Toxicity of verapamil
hypotension, AV block, worsening of CHF, bradycardia
Interactions of verapamil
additive effects with most other antihypertensives; additive toxic effects on heart when given with beta-blockers
Special considerations of verapamil
use reduced doses in patients with both renal and hepatic disease; short-acting nifedipine (and similar CEBs) can increase risk of MI (unclear why); Pregnancy C
Indications and dose/route for verapamil
80mg thrice daily, or 240 mg SR once daily
Monitoring of verapamil
hypotension, orthostasis, worsening CHF or conduction